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Pharm 845 Exam #3 > Muscle Relaxants & Ethanol- Dr. Masserano > Flashcards

Muscle Relaxants & Ethanol- Dr. Masserano Flashcards

1
Q

Examples of acute muscle spasm

A

-Lower back pain
-Neck pain
-Tension headache
-TMJ
(Treat with Antispasmodic drugs)

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2
Q

Examples of chronic conditions

A

-Cerebral palsy
-Multiple sclerosis
-Spinal cord injury
-Stroke
-Fibromyalgia
-Myofascial pain syndrom
(Treat with antispasticity drugs)

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3
Q

When to use antispasmodic agents

A

-Musculoskeletal conditions

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4
Q

When to use antispasticity agents

A

-Upper motor neuron disorders

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5
Q

List some antispasmodic agents

A
  • Cyclobenzaprine
  • Methocarbamol
  • Carisoprodol
  • Chlorzoxazone
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6
Q

List some anti spastic agents

A
  • Baclofen (safe in elderly)

- Dantrolene

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7
Q

Which two agents have both antispastic and antispasmodic properties

A
  • Diazepam

- Tizanidine (safe in elderly)

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8
Q

What are 1st, 2nd, and 3rd line treatment options for both acute and chronic lower back pain

A 
Acute pain
-1st line: Tylenol/NSAIDs
-2nd line: Skeletal muscle relaxants
-3rd line: Opioids
Chronic pain 
-1st line: Tylenol/ NSAIDs
-2nd line: TCAs/SNRIs
-3rd line: Skeletal muscle relaxants/ opioids
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9
Q

Diazepam (Valium) MoA

A
  • Potentiates GABA hyperpolarization (Cl- channel) by action on the GABAa receptor
  • Site of action: CNS and Spinal cord
  • Treats antispasticity and antispasmodic disorders
  • Sedation: Main side effect
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10
Q

Baclofen (Lioresal)

A
  • Derivative of GABAb
  • Decreases calcium influx and transmitter release (decreasing glutamate)
  • Increases K+ efflux (Hyperpolarizing)
  • Recommended for treatment of spasticity
  • Do NOT abruptly DC, gradually reduce the dose
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11
Q

Tizanidine (Zanaflex)

A
  • Alpha 2 agonist
  • Decreases calcium flow into presynaptic neuron
  • Decreasing glutamate release
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12
Q

Dantrolene (Dantrium)

A
  • Inhibits RyR1 channel in skeletal muscle
  • Inhibits calcium release intracellularly
  • Thus inhibiting contractions
  • Treatment for spasticity
  • Also can treat malignant hyperthermia
  • No effect on cardiac/smooth muscle (RyR2 is found here)
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13
Q

Black box warning with Dantrolene (Dantrium)

A
  • Discontinue if no benefit with in 45 days

- Potential for hepatotoxicity

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14
Q

What do alpha 2 agonists do

A
  • Decrease Ca++ uptake

- Decreasing glutamate release

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15
Q

Cyclobenzaprine (Flexril, Amrox) MoA

A
  • Works on upper CNS
  • Alpha 2 agonist
  • 5HT2 antagonist
  • May prolong QT interval
  • Potential for serotonin syndrome (when combined with TCAs, SSRIs, SNRIs, MAOIs)
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16
Q

Carisoprodol (Soma) MoA and drug schedule

A
  • Schedule IV
  • Do not combine with other CNS depressants
  • Potential for drug abuse, dependence, and withdrawal
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17
Q

Methocarbamol (Robaxin) MoA

A
  • CNS depressant
  • Treats acute musculoskeletal pain
  • Can cause sedation
18
Q

Palcohol

A
  • Freeze dried alcohol
  • Federally legal
  • Illegal in many states
  • Exceptions: NM and CO
19
Q

CNS depression increases with more or less hydrocarbons?

A
  • Increase hydrocarbons = increased CNS depression

- Isopropanol > Ethanol> Methanol

20
Q

Who will have a higher blood alcohol level; an obese patient or an healthy patient

A
  • The obese patient
  • Distributed though water
  • Increased fat content = decreased water content
21
Q

What is the value of “r” in men vs women

A
  • Men = 0.68

- Women = 0.55

22
Q

How many grams of ethanol is in one standard drink?

A

-14.4 grams

23
Q

What type of kinetics does ETOH follow?

A
  • Zero order kinetics

- One drink takes about 1.5 to 2hrs to be eliminated

24
Q

What enzymes are involved in the metabolism of ETOH

A
  • Alcohol dehydrogenase

- Aldehyde dehydrogenase

25
Why are asians light weights?
- Higher Km for aldehyde (lower activity) - Making them slower metabolizers - Build up of aldehyde levels lead to poor side effects - Deters these people from drinking
26
What are some effects of ETOH on the body
- Lactate acidosis - Hyperlipidemia - Severe liver damage - Hypoglycemia
27
What is the use of fructose in alcohol overdose
- May help to rapidly reoxidize NADH to NAD - Increasing the metabolism of alcohols metabolites - Can increase the metabolism by up to 20%
28
CNS effects of ETOH
- Sedation - Anticonvulsant - Analgesic - Sleep effects
29
Total body effects of chronic ETOH ingestion
- Liver damage - GI tract issues - Muscle damage - Heart/CV effects - Kidney - CNS
30
Positive effects of ETOH use in MODERATION
- Decreases CV risk - Improves lipid profile - Makes blood vessels healthier - Decreases BP - Decreases inflammation
31
Wernicke-Korsakoff syndrome
``` -Due to malabsorption of thiamine (B1) Wernicke's disease: -Opthalmic difficulties -Ataxia of gait -Disoriented Treatment: supplement with B1 ```
32
How do you treat methanol and ethylene glycol poisoning
-Competitively block alcohol dehydrogenase
33
What is Denatonium Benzoate
- Additive to antifreeze | - Makes it taste bitter so your dog wont eat it
34
MoA of Fomepizole (Antizol)
- Injection that competitively inhibits alcohol dehydrogenase - Used in treatment of methanol/ethylene glycol poisoning - Used in combo with hemodialysis and general supportive care
35
Acute drug ints with ETOH
Increases the half life of: - Warfarin - Tylenol
36
Drug ints with chronic ETOH
- Decreases half life of Tylenol | - Increases toxic quinone when ETOH leaves system
37
Tylenol and ETOH better explained
- Tylenol is metabolized by CYP2E1 to a toxic quinone - Ethanol competes with Tylenol (induces CYP2E1) - Once ETOH is eliminated the production of toxic quinone is increased (due to upregulation of CYP2E1)
38
Disulfiram (Antabuse)
-Blocks the conversion of acetaldehyde to acetic acid by inhibiting aldehyde dehydrogenase
39
Naltrexone (Revia)
- Long acting opioid antagonist - Helps to reduce relapse rates in alcoholics - Diminishes the "high" of ETOH
40
Acamprosate (Campral)
- Blocks glutamatergic N methyl D asparte receptors - While activating GABAb receptors - Must be abstinent from ETOH at the initiation of treatment
41
Varenicline (Chantix)
- Helps to reduce alcohol consumption and alcohol cravings | - Best for pts that are also trying to quit smoking

Pharm 845 Exam #3 (7 decks)

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